SYNTHESIS, CHARACTERIZATION, AND ANTHELMINTIC ACTIVITY OF NOVEL BENZOTHIAZOLE DERIVATIVES CONTAINING INDOLE MOIETIES

  • ALETI RAJAREDDY Department of Pharmaceutical Chemistry, Mall Reddy Pharmacy College, Secunderabad, Telangana, India,
  • SRINIVAS MURTHY M Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Deshmukhi, Telangana, India.

Abstract

Objective: The objective of this study was to synthesize and evaluate the anthelmintic activity (AA) of novel benzothiazole derivatives containing indole moieties (BDIM).


Methods: The present works which involve the substituted isatin Schiff bases undergo acetylating and reacting with 2-aminobenzothiazole to give novel BDIM.


Results: All the newly synthesized molecules (5a-5o) were characterized by Fourier-transform infrared spectroscopy, H_nuclear magnetic resonance, and mass spectral analysis along with physical data. The biological potentials of the newly synthesized compounds are evaluated for their AA using an Indian earthworm (Pheretima posthuma), and albendazole was used as standard drug.


Conclusion: The synthesized compound 5f, 5n, and 5o showed good AA, whereas others exhibited significant activities.

Keywords: Substituted benzaldehyde, Isatin, p-Toluidine, 2-aminobenzothiazole, Anthelmintic activity.

References

1. Catalano A, Desaphy JF, Lentini G, Carocci A, Di Mola A, Bruno C, et al. Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels. J Med Chem 2012;55:1418-22.
2. Carocci A, Catalano A, Lovece A, Lentini G, Duranti A, Lucini V, et al. Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors. Bioorg Med Chem 2010;18:6496-511.
3. Baell JB, Duggan PJ, Forsyth SA, Lewis RJ, Lok YP, Schroeder CI, et al. Synthesis and biological evaluation of nonpeptide mimetics of omega-conotoxin GVIA. Bioorg Med Chem 2004;12:4025-37.
4. Gaware VM, Dhamak KB, Kotade KB. Synthesis and evalution of benzothiazole derivatives for anthelmintic activity. Eur J Pharm Med Res 2016;3:454-9.
5. Cavalluzzi MM, Bruno C, Lentini G, Lovece A, Catalano A, Carocci A, et al. One-step synthesis of homochiral O-aryl and O-heteroaryl mandelic acids and their use as efficient 1H NMR chiral solvating agents. Tetrahedron Asymmetry 2009;20;1984-91.
6. Siddiqui N, Rana A, Khan SA, Bhat MA, Haque SE. Synthesis of benzothiazole semicarbazones as novel anticonvulsants the role of hydrophobic domain. Bioorg Med Chem Lett 2007;17:4178-82.
7. Kaur H, Kumar S, Singh I, Saxena KK, Kumar A. Synthesis, characterization and biological activity of various substituted benzothiazole derivatives. Dig J Nanomater Biostruct 2010;5:67-76.
8. Leena KP, Subin MZ, Deepthy CH. In silico design, synthesis and characterization of some novel benzothiazole derivatives as anticancer agents. Asian J Pharm Clin Res 2017;10:50-15.
9. Mohammed JM. Synthesis, characterization and preliminary antimicrobial evaluation of new Schiff bases of ampicillin and amoxicillin derived from isatin derivatives. Int J Pharm Pharm Sci 2016;8:113-6.
10. Ajaiyeoba EO, Onocha PA, Olarenwaju OT. In vitro anthelmintic properties of Buchholzia coriaceae and Gynandropsis gynandra extract. Pharm Biol 2001;39:217-20.
11. Maneshwar T, Krishna M, Vijetha N. Synthesis, characterization and biological evaluation of novel benzimidazole derivatives. J Pharm Res 2015;4:188-92.
12. Himaja M, Sirisha B, Moonjit D, Munirasekhar D. Synthesis and anthelmintic activity studies of 1-substituted benzimidazole derivatives. J Indian Chem Soc 2015;92:908-10.
Statistics
14 Views | 87 Downloads
How to Cite
RAJAREDDY, A., and S. MURTHY M. “SYNTHESIS, CHARACTERIZATION, AND ANTHELMINTIC ACTIVITY OF NOVEL BENZOTHIAZOLE DERIVATIVES CONTAINING INDOLE MOIETIES”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 3, Feb. 2019, pp. 321-5, https://innovareacademics.in/journals/index.php/ajpcr/article/view/30530.
Section
Original Article(s)